e-Drug3D

1471

ILOPERIDONE

INN
ILOPERIDONE

cas 133454-47-4

CLASS

ANTIPSYCHOTIC
DOPAMINE ANTAGONIST
SEROTONIN ANTOGONIST
SCHIZOPHRENIA
NERVOUS SYSTEM
SEROTONIN 5-HT2A DOPAMINE D2 AND D3 RECEPTORS (KI VALUES OF 5.6, 6.3, 7.1,NM, RESPECTIVELY). MODERATE AFFINITY FOR DOPAMINE D4, SEROTONIN 5-HT6 AND 5-HT7RECEPTORS AND NOREPINEPHRINE NEAPLHA1 RECEPTORS (KI VALUES OF 25, 43, 22, AND 36 NM RESPECTIVELY), AND LOW AFFINITY FOR THE SEROTONIN 5HT1A, DOPAMINE D1, AND HISTAMINE H1 RECEPTORS (KI VALUES OF 168, 216 AND 473 NM, RESPECTIVELY). NO APPRECIABLE AFFINITY (KI>1000 NM) FOR CHOLINERGIC MUSCARINIC RECEPTORS.

ROUTE (list)

ORAL

ATC code

N05AX14

PK parameters

VD 2070 LITER
Cl 74.5 LITER / HOUR
PPB 95 PERCENT
t1/2 18 HOUR

Solubility

PRACTICALLY INSOLUBLE IN WATER

Target

TARGET DOPAMINE D2 (KI = 6.3 NANOMOLAR)
SEROTONIN 5-HT2A (KI = 5.6 NANOMOLAR)
DOPAMINE D3 (KI = 7.1 NANOMOLAR)

DrugCentral

D(2) dopamine receptor UNIPROT P14416 DRD2

5-hydroxytryptamine receptor 2A UNIPROT P28223 HTR2A

Download SDF file

1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1- piperidinyl]propoxy]-3-methoxyphenyl]ethanone

Formula:
C24H27FN2O4

Calculated chemical properties:

MW 426.48
NB_atoms 31
XLogP 4.83
PSA 68.947
NB_HD 0
NB_HA 6
fsp3 0.42
Lipinski(0=no;1=yes) 1

FDA
NDA 022192 (pdf not found) INN (ILOPERIDONE) FANAPT (VANDA PHARMS INC) APPROVAL= AP YEAR= 2009
NDA 207231 (pdf not found) INN (ILOPERIDONE) ILOPERIDONE (INVENTIA) APPROVAL= AP YEAR= 2016 DISCONTINUED
NDA 207409 (pdf not found) INN (ILOPERIDONE) ILOPERIDONE (ALEMBIC PHARMS LTD) APPROVAL= TA YEAR= 2018
NDA 207098 (pdf not found) INN (ILOPERIDONE) ILOPERIDONE (TARO) APPROVAL= AP YEAR= 2019 DISCONTINUED
NDA 206890 (pdf not found) INN (ILOPERIDONE) ILOPERIDONE (LUPIN LTD) APPROVAL= AP YEAR= 2022 DISCONTINUED